C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 217/26 (2006.01) A61K 31/47 (2006.01) C07K 5/078 (2006.01) A61K 38/00 (2006.01)
Patent
CA 2251647
Substituted isoquinoline-3-carboxamides, their preparation and their use as pharmaceuticals Novel isoquinoline-3-carboxamides of the formula I (see formula I) in which R1 is hydrogen or chlorine, R2 is hydrogen, alkyl, alkoxy, chlorine, trifluoromethyl, hydroxyl, or benzyloxy which is optionally substituted, or fluoroalkoxy of the formula O-[CH2]x-C f H(2f+1-g)Fg where x = 0 or 1, f= 1- 5 and g = 1 to (2f+1), R3 is hydrogen, alkyl, alkoxy, fluorine, chlorine, cyano, trifluoromethyl, hydroxyl, or benzyloxy which is optionally substituted, or fluoroalkoxy of the above formula, R4 and R5 are hydrogen, alkyl, fluorine, chlorine, bromine, trifluoromethyl, cyano, alkoxy, or fluoroalkoxy of the above formula, including the physiologically active salts, are strong prolyl-4-hydroxylase inhibitors which do not cause steatosis.
L'invention porte sur des isoquinoline-3-carboxamides substitués, leur préparation et leur utilisation en tant que produits pharmaceutiques. Les nouveaux isoquinoline-3-carboxamides présentent la formule I (voir formule I) dans laquelle R1 est un hydrogène ou un chlore, R2 est un hydrogène, un alkyle, un alkoxy, un chlore, un trifluorométhyl, un hydroxyle ou un benzyloxy qui est facultativement substitué, ou un fluoroalkoxy de formule O-¬CH2|x-C f H(2f+1-g)Fg où x = 0 ou 1, f = 1- 5 et g = 1 à (2f+1), R3 est un hydrogène, un alkyle, un alkoxy, un fluor, un chlore, un cyano, un trifluorométhyl, un hydroxyle ou un benzyloxy qui est facultativement substitué, ou un fluoroalkoxy ayant la formule donnée précédemment, R4 et R5 sont un hydrogène, un alkyle, un fluor, un chlore, un brome, un trifluorométhyle, un cyano, un alkoxy ou un fluoroalkoxy de la formule mentionnée précédemment, y compris les sels physiologiquement actifs. Ces nouveaux composés sont des inhibiteurs puissants de la prolyl-4-hydroxylase, qui ne causent pas de stéatose.
Baringhaus Karl-Heinz
Tschank Georg
Weidmann Klaus
Werner Ulrich
Bereskin & Parr Llp/s.e.n.c.r.l.,s.r.l.
Fibrogen Inc.
Hoechst Marion Roussel Deutschland Gmbh
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